Process for preparing anti-cancer medicine Exemestane

A technology for exemestane and a compound is applied in the field of improvement of the synthesis process of anticancer drug exemestane, can solve the problems of low yield, expensive raw materials, environmental pollution and the like, and achieves simple operation, convenient post-processing and cost reduction Effect

Inactive Publication Date: 2007-03-14
SHANGHAI HUATUO MEDICAL SCI CO LTD
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Problems solved by technology

[0010] The purpose of the invention is to overcome the disadvantages of expensive raw materials, low yield and environmental pollution in the prior art, and provide a method for synthesizing exemestane with relatively cheap raw materials, high yield, simple operation and reduced environmental pollution. method

Method used

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  • Process for preparing anti-cancer medicine Exemestane
  • Process for preparing anti-cancer medicine Exemestane
  • Process for preparing anti-cancer medicine Exemestane

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Embodiment Construction

[0026] The present invention will be further described below in conjunction with specific examples, but the present invention is not limited.

[0027] 1. Preparation of dehydrogenation reagent o-iodobenzoic acid II: 13.5 g of o-iodobenzoic acid, 85 ml of sulfuric acid (8N) and 50 ml of glacial acetic acid were added, heated to boil, and the mixture was dissolved. A solution of 8.4 g of potassium bromate in 85 ml of hot water was then added dropwise. The generated bromine vapor was absorbed with aqueous sodium hydroxide solution. It can be observed that the reaction solution is gradually cloudy and crystal precipitation occurs. The addition was completed within 1 hour and then refluxed for 2 hours after the addition was complete. The reactant was cooled, poured into ice water, filtered, washed with 300 ml of water, and then washed with chloroform to obtain 14.5 g of silver-white crystals. MP = 220°C (decomposition), yield: 95%.

[0028] 2, Synthesis of 6-methylene-androst-4...

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Abstract

The present invention provides a preparation process of anticancer medicine Exemestane. Androstene-4-ene-3, 17-dione as initial material and trialkyl orthoformate react under the action of the catalyst to produce enol ether, enol ether is then reacted with N-methylaniline and formaldehyde, and the reaction product is made to react with dehydrogenating agent IBX in inert solvent and under the protection of inert gas at certain temperature to obtain Exemestane. The said method is simple and convenient in post-treatment, has no environmental pollution and low cost and is suitable for industrial production.

Description

technical field [0001] The present invention relates to organic synthesis, and more specifically refers to an improved synthesis process of anticancer drug exemestane. technical background [0002] Breast cancer is the most common malignancy in women. With the change of lifestyle and environment, more and more women are married late or have no childbirth or breastfeeding after marriage, and the incidence of breast cancer is increasing year by year. According to statistics, the incidence of breast cancer has jumped from the seventh place 10 years ago to the first place in the incidence of female tumors. In the United States, the death rate of breast cancer is second only to lung cancer, ranking second. [0003] At present, effective treatment methods for breast cancer include surgery, chemotherapy, radiotherapy, etc. In recent years, more and more attention has been paid to anti-estrogen therapy for breast cancer, especially in the treatment of advanced breast cancer. [0...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J1/00
Inventor 朱勤潘俊芳
Owner SHANGHAI HUATUO MEDICAL SCI CO LTD
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